Antioxidant and cytoprotective properties of loganic acid isolated from seeds of Strychnos potatorum L. against heavy metal induced toxicity in PBMC model.

Present work carried out with the objectives to isolate active component of S. potatorum and also to evaluate its free radical scavenging activity and preventing capacity against heavy metal toxicity. Solvents of different polarity were used to prepare crude extracts of S. potatorum seeds and screened for antioxidant activity. Among the crude extracts, methanolic extract was found to exhibit higher antioxidant activity (81.22%) which was fractionated by liquid-liquid partitioning method. Among the different fractions (LF1-LF4), LF-2 showed higher antioxidant activity (98.24%) as compared to other three liquid fractions and hence LF-2 was further purified by column chromatography. Among nine column fractions (CF1-CF9), fraction CF-7 was found to have higher antioxidant activity (92.14%), which was further analyzed using LC-MS and NMR and identified as loganic acid. In vitro radical scavenging assays showed remarkable antioxidant activity of loganic acid in terms of DPPH scavenging (IC50 149 µg/ml), superoxide radical scavenging (IC50 632.43 µg/ml) and hydroxyl radical scavenging (IC50 29.78 µg/ml). Loganic acid exhibited 81% prevention of heavy metal toxicity through the mechanism of inhibiting ROS generation (2046 AU vs. 5264 AU in control) and lipid peroxidation (95.01%). Thus, the active compound (loganic acid) isolated from S. potatorum has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity.

Plant phenyl-propanoids-conjugated silver nanoparticles from edible plant Suaeda maritima (L.) dumort. Inhibit proliferation of K562-human myeloid leukemia cells.

The present study portrays the isolation of four phenylpropanoids - ferulic acid (FA), sinapic acid (SA), caffeic acid (CA), and chlorogenic acid (CHA) from the water extract of Suaeda maritima (L.) Dumort, a phytochemically less explored Indian medicinal plant. Further, synthesis and characterization of silver and gold nanoparticles using the isolated phenylpropanoids were done. The silver nanoparticles synthesized from S. maritima water extract along with silver nano-conjugated forms of the isolated compounds exhibited appreciable anti-leukemic activity against K562 cells (human myeloid leukemia). Especially, the ferulic and CA-conjugated silver nanoparticles showed significant (P < .01) activity against leukemia.

Studies on physicochemical and nutritional properties of aerial parts of Cassia occidentalis L.

In the present, work chemical composition and nutritional value of aerial parts of Cassia occidentalis L. was studied. The aerial parts of C. occidentalis possess favorable physicochemical properties with good nutritional value, such as high energy value, crude fibers, and vitamin levels. The X-ray fluorescence spectrophotometry data revealed that the sample is rich in minerals, especially in Fe, Ca, K, and Mn. Further, minerals such as Mg, Zn, Cu, Na, P, and S are present in good amount and depicted the nutritional value of the selected material. The plant sample is rich in phytochemicals such as flavonoids, alkaloids, lignin, tannins, and phenols. The presence of phytochemical constituents was confirmed by gas chromatography-mass spectrometry profile and high-performance thin layer chromatography fingerprinting techniques. The findings stimulate the on-farm cultivation of C. occidentalis on a large scale to relieve the iron deficiency in local community, and it can be used as a dietary supplement to treat anemia.

Aqueous and alcoholic extracts of Triphala and their active compounds chebulagic acid and chebulinic acid prevented epithelial to mesenchymal transition in retinal pigment epithelial cells, by inhibiting SMAD-3 phosphorylation.

Epithelial to Mesenchymal Transition (EMT) of the retinal pigment epithelium is involved in the pathogenesis of proliferative vitreoretinopathy (PVR) that often leads to retinal detachment. In this study, Triphala, an ayurvedic formulation and two of its active ingredients, namely chebulagic acid and chebulinic acid were evaluated for anti-EMT properties based on in vitro experiments in human retinal pigment epithelial cell line (ARPE-19) under TGFß1 induced conditions. ARPE-19 cells were treated with TGFß1 alone or co-treated with various concentrations of aqueous extract (AqE) (30-300 µg/ml); alcoholic extract (AlE) (50-500 µg/ml) of triphala and the active principles chebulagic acid (CA) and chebulinic acid (CI) (CA,CI: 50-200 µM). The expression of EMT markers namely MMP-2, αSMA, vimentin and the tight junction protein ZO-1 were evaluated by qPCR, western blot and immunofluorescence. The functional implications of EMT, namely migration and proliferation of cells were assessed by proliferation assay, scratch assay and transwell migration assay. AqE, AlE, CA and CI reduced the expression and activity of MMP-2 at an ED50 value of 100 µg/ml, 50 µg/ml, 100 µM and 100 µM, respectively. At these concentrations, a significant down-regulation of the expression of αSMA, vimentin and up-regulation of the expression of ZO-1 altered by TGFß1 were observed. These concentrations also inhibited proliferation and migration of ARPE-19 cells induced by TGFß1. EMT was found to be induced in ARPE-19 cells, through SMAD-3 phosphorylation and it was inhibited by AqE, AlE, CA and CI. Further studies in experimental animals are required to attribute therapeutic potential of these extracts and their active compounds, as an adjuvant therapy in the disease management of PVR.

Pharmacodynamic studies on the isolated active fraction of Acacia farnesiana (L.) willd.

BACKGROUND: Acacia farnesiana is a medicinal plant that grows throughout tropical parts of Indian subcontinent, particularly in sandy soils of river beds in Northern India. The objective of the present study was to evaluate the anti-hyperglycemic activity of the extracts using glucose tolerance test. Isolation of an active fraction (AF) from the active extract (water extract) using alcohol precipitation and to get insight to the mechanism of action of the AF of A. farnesiana. MATERIALS AND METHODS: Glucose uptake by isolated rat diaphragm of the AF was performed. Further the effect of release of Insulin from isolated and cultured pancreatic ß-cell was determined. Besides, effect of oral administration of the AF was compared with that of intraperitonial administration. The effect of AF on serum glucose levels in orally glucose loaded rats was compared with that of intraperitoneal glucose loaded rats. RESULTS: The water extract significantly lowered the blood glucose level. When precipitated with alcohol, the activity was found in the soluble fraction. Glucose uptake in the isolated rat hemidiaphragm, was increased by the AF at 40 µg/ml concentration, the AF did not significantly influence insulin release from cultured islets. The AF was found to be effective in orally glucose loaded in contrast to intraperitonial route. CONCLUSION: Our findings suggest that this plant is promising for further studies leading to the development of valuable medicine for diabetes.

Pogostemon hirsutus oil, rich in abietane diterpenes.

Volatile oil extracted from the leaves of Pogostemon hirsutus Benth., a rare species from Anamalai hills of the Western Ghats of Tamil Nadu, India was analyzed by GC-FID and GC-MS. Fifty-four compounds amounting to 90.8% of the oil were identified. The oil was rich in monoterpenes and diterpenes. The major components of the oil were alpha-pinene (11.5%), sabinene (8.5%), beta-pinene (5.2%), abietatriene (16.3%), dehydroabietal (3.5%) and dehydroabietol (21.0%). Abietane diterpenes are reported for the first time in the genus Pogostemon of Lamiaceae with six abietanes representing 42.6% of the oil.

Isolation and in silico evaluation of antidiabetic molecules of Cynodon dactylon (L.).

Cynodon dactylon is a potential source of metabolites such as flavanoids, alkaloids, glycosides and ß-sitosterol and has been traditionally employed to treat urinary tract and other microbial infections and dysentery. The present work attempts to evaluate the activity of C. dactylon extracts for glycemic control. Aqueous extracts of C. dactylon analyzed by HPLC-ESI MS have identified the presence of apigenin, luteolin, 6-C-pentosyl-8-C-hexosyl apigenin and 6-C-hexosyl-8-C-pentosyl luteolin. Evaluation of hypoglycemic activity through an extensive in silico docking approach with PPARγ (Peroxisome Proliferator-Activated Receptor), GLUT-4 (glucose transporter-4) and SGLT2 (sodium glucose co-transporter-2) revealed that luteolin, apigenin, 6-C-pentosyl-8-C-hexosyl apigenin, 6-C-hexosyl-8-C-pentosyl luteolin interact with SGLT2. Interactions of these molecules with Gln 295 and Asp 294 residues of SGLT2 have been shown to compare well with that of the phase III drug, dapagliflozin. These residues have been proven to be responsible for sugar sensing and transport. This work establishes C. dactylon extract as a potential SGLT2 inhibitor for diabetic neuropathy thus enabling a possibility of this plant extract as a new alternative to existing diabetic approaches.